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Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.

ABSTRACT: N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs.

SUBMITTER: Kindon N

PROVIDER: S-EPMC5601455 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.

Kindon Nicholas N Andrews Glen G Baxter Andrew A Cheshire David D Hemsley Paul P Johnson Timothy T Liu Yu-Zhen YZ McGinnity Dermot D McHale Mark M Mete Antonio A Reuberson James J Roberts Bryan B Steele John J Teobald Barry B Unitt John J Vaughan Deborah D Walters Iain I Stocks Michael J MJ

ACS medicinal chemistry letters 20170901 9

<i>N</i>-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide <b>1</b> was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate dru ...[more]

PMID: 28947948

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